Reaction Details Report a problem with these data
Target
Glutamate receptor 1
Ligand
BDBM213888
Substrate
n/a
Meas. Tech.
Two-electrode Voltage Clamp Electrophysiology
pH
7.4±n/a
Temperature
298.15±n/a K
Ki
>1.80e+5±n/a nM
IC50
>3.00e+5±n/a nM
Comments
extracted
Citation
 Kvist, T; Steffensen, TB; Greenwood, JR; Mehrzad Tabrizi, F; Hansen, KB; Gajhede, M; Pickering, DS; Traynelis, SF; Kastrup, JS; Bräuner-Osborne, H Crystal structure and pharmacological characterization of a novel N-methyl-D-aspartate (NMDA) receptor antagonist at the GluN1 glycine binding site. J Biol Chem 288:33124-35 (2013) [PubMed]  Article 
Target
Name:
Glutamate receptor 1
Synonyms:
AMPA-selective glutamate receptor 1 | GRIA1_RAT | GluA1 | GluR-1 | GluR-A | GluR-K1 | Glur1 | Glutamate receptor ionotropic, AMPA 1 | Gria1
Type:
Protein
Mol. Mass.:
101583.91
Organism:
Rattus norvegicus (Rat)
Description:
P19490
Residue:
907
Sequence:
MPYIFAFFCTGFLGAVVGANFPNNIQIGGLFPNQQSQEHAAFRFALSQLTEPPKLLPQIDIVNISDSFEMTYRFCSQFSKGVYAIFGFYERRTVNMLTSFCGALHVCFITPSFPVDTSNQFVLQLRPELQEALISIIDHYKWQTFVYIYDADRGLSVLQRVLDTAAEKNWQVTAVNILTTTEEGYRMLFQDLEKKKERLVVVDCESERLNAILGQIVKLEKNGIGYHYILANLGFMDIDLNKFKESGANVTGFQLVNYTDTIPARIMQQWRTSDSRDHTRVDWKRPKYTSALTYDGVKVMAEAFQSLRRQRIDISRRGNAGDCLANPAVPWGQGIDIQRALQQVRFEGLTGNVQFNEKGRRTNYTLHVIEMKHDGIRKIGYWNEDDKFVPAATDAQAGGDNSSVQNRTYIVTTILEDPYVMLKKNANQFEGNDRYEGYCVELAAEIAKHVGYSYRLEIVSDGKYGARDPDTKAWNGMVGELVYGRADVAVAPLTITLVREEVIDFSKPFMSLGISIMIKKPQKSKPGVFSFLDPLAYEIWMCIVFAYIGVSVVLFLVSRFSPYEWHSEEFEEGRDQTTSDQSNEFGIFNSLWFSLGAFMQQGCDISPRSLSGRIVGGVWWFFTLIIISSYTANLAAFLTVERMVSPIESAEDLAKQTEIAYGTLEAGSTKEFFRRSKIAVFEKMWTYMKSAEPSVFVRTTEEGMIRVRKSKGKYAYLLESTMNEYIEQRKPCDTMKVGGNLDSKGYGIATPKGSALRNPVNLAVLKLNEQGLLDKLKNKWWYDKGECGSGGGDSKDKTSALSLSNVAGVFYILIGGLGLAMLVALIEFCYKSRSESKRMKGFCLIPQQSINEAIRTSTLPRNSGAGASGGGGSGENGRVVSQDFPKSMQSIPCMSHSSGMPLGATGL
  
Inhibitor
Name:
BDBM213888
Synonyms:
1-thioxo-1,2-dihydro-[1,2,4]triazolo[4,3-a]-quinoxalin-4(5H)-one | TK40
Type:
Small organic molecule
Emp. Form.:
C9H6N4OS
Mol. Mass.:
218.235
SMILES:
Sc1nnc2n1c1ccccc1[nH]c2=O
Structure:
Search PDB for entries with ligand similarity: